Fractionation of a chalone-containing preparation from Ehrlich's ascites tumor by high performance liquid chromatography

Department of Biology, Medico-Biological Faculty, and Applied Research Laboratory of Ecology, Toxicology, and Metabolism of Medicinal Preparations, attached to the Department of Biochemistry, Medico-Biological Faculty, N. I. Pirogov Second Moscow Medical Institute. Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 112, No. 10, pp. 418–419, October, 1991.     

Synthesis of 3-(3-pyridyl)- and 3-(3-benzo[b]thienyl)-D-alanine

The DL-arylamino acid ethyl ester derivatives of β-(3-pyridyl)-DL-alanine, and β-(3-benzo[b]thienyl)-DL-alanine were synthesized by diethyl acetamidomalonate condensation with the respective arylmethyl halides followed by partial hydrolysis to the monoethyl ester and decarboxylation. Each derivative was enzymatically resolved to a separable mixture of the corresponding N-acetyl-L-amino acid and the unchanged D amino acid derivative. Acidic hydrolysis of the latter gave the corresponding D-amino acid, the optical purity of which was established by HPLC analysis of the 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate (GITC) derivative. The free D amino acids were converted to D-BOC derivatives by reaction with di-tert-butyldicarbonate in tert-butyl alcohol, water and sodium hydroxide.     

Intrathecal synthesis of IgG subclasses in multiple sclerosis and in acquired immunodeficiency syndrome (AIDS)

Serum and cerebrospinal fluid (CSF) of 50 neurological patients (24 multiple sclerosis (MS), ten acquired immunodeficiency syndrome (AIDS) and 16 other neurological diseases (OND)) and ten controls were analyzed by enzyme-linked immunosorbent assay (ELISA) for IgG subclass quantification and for the calculation of intrathecal synthesis (ITS). Total IgG was determined by two methods: electroimmunodiffusion (EID) and ELISA. A highly significant correlation was established between both methods. The existence of ITS was proved by the IgG/albumin ratio, the IgG index, Tourtellotte's formula, and Schuller's formula. In AIDS patients all IgG subclasses showed an increase in the CSF, whereas in sera only the IgG1 was significantly increased. CSF of MS patients showed a predominant increase of IgG1 whereas no significant modification of IgG subclasses was observed in sera. In most of the AIDS patients there was an ITS of IgG1, IgG3 and IgG4, but rarely (3/10) IgG2. In contrast, a polyclonal ITS of IgG was exceptional (1/24) in MS patients. No significant correlation could be established between clinical data and IgG subclass ITS in MS. The variations of each IgG subclass in serum and in ITS were not significantly correlated. Measurement of each IgG subclass and calculation of ITS seems essential in order to analyze any subclass antibody repertory inside the central nervous system.     

Two-step hard acid deprotection/cleavage procedure for solid phase peptide synthesis

A new two-step deprotection/cleavage procedure for t-butoxycarbonyl (Boc) based solid phase peptide synthesis is reported. First the protective groups are removed from 4-(oxymethyl)-phenylacetamidomethyl (PAM) resin attached peptide with the weak hard acid, trimethylsilyl bromide-thioanisole/trifluoroacetic acid (TFA). In the second step, the peptide is cleaved from the resin with a stronger hard acid such as trimethylsilvl trifluoromethanesulfonate in TFA or with HF. The method is also shown to deformylate Nⁱⁿ-formyltryptophan moiety efficiently. The usefulness of this procedure for practical solid phase peptide synthesis is demonstrated by comparison with other deprotection methods in the synthesis of urotensin II and human endothelin.     

麦冬对甲基磺酸甲酯诱发的小鼠精子非程序DNA合成的抑制作用

目的:观察中草药麦冬对雄性小鼠生殖细胞遗传物质损伤的防护作用.方法:采用雄性小鼠生殖细胞非程序DNA合成实验.结果:麦冬各剂量组诱导的非程序DNA合成与正常对照组比较差异无显著性(P>0.05);6.8～13.6 g*kg-1剂量,麦冬对甲基磺酸甲酯所诱导的非程序DNA合成有明显抑制作用(P<0.01),并且随着麦冬浓度的增加,其抑制作用逐渐增强,超过一定剂量,其抑制作用不再增强.结论:麦冬对小鼠生殖细胞遗传物质具有保护作用.     

消旋17-苯-18,19,20-失三碳前列腺素F2α甲酯及其15-差向异构体的合成

从中间体(4)出发,经醛(5),与鏻叶立德(3)或2-酮-4-苯丁烷磷酸酯(11)钠缩合成(6),再钠硼氢还原得3′α-醇(7A)及其差向异构体(7B),经硅胶柱色谱分开,分别经二异丁基铝氢还原,与溴化5-三苯鏻戊酸之Wittig试剂缩合,得17-苯-18,19,20-失三碳前列腺素F_2α(9A)及其15-差向异构体(9B),再用重氮甲烷甲酯化,分别得相应的17-苯-18,19,20-失三碳前列腺素F_2α甲酯(10A)及其15-差向异构体(10B)。     

人胚呼吸道上皮细胞非时序DNA合成

为研究和比较化学致癌物对人呼吸道上皮细胞和纤维母细胞的损伤及损伤后DNA修复合成的差异,作者用直接致癌物4-硝基喹啉-1-氧化物(4-NQO)和间接致癌物3,4-苯并芘(BaP)处理人胚鼻咽、气管上皮细胞和纤维母细胞,用放射自显影术测定这3种细胞的非时序脱氧核糖核酸合成(UDS)。用4-NQO处理后,这3种细胞的UDS均呈明显的剂量依赖(dose dePendency)关系,但气管和鼻咽上皮细胞UDS平均分别是纤维母细胞的3.0和2.4倍。用BaP处理后,气管和鼻咽上皮细胞UDS呈现明显的剂量依赖关系,而纤维母细胞未见这种关系。气管和鼻咽上皮细胞的UDS平均分别是纤维母细胞的8.6和3.0倍。     

中位含氯取代环己烯桥环硫三碳菁染料的合成及性能

采用2-甲基噻唑季胺盐与2-氯-1-甲酰基3-羟亚甲基环己烯,合成了五种题示染料。经IR及~1H-NMR谱确认了产物的结构,测定了电子吸收光谱、溶解度及稳定性,发现在染料苯环上引入甲氧基能改进染料溶解度,苯环上有氯取代的染料具有较高的光稳定性。     

Effect of dipyridamole with or without aspirin on urine protein excretion in patients with membranous glomerulonephritis

Summary The antiproteinuric effect of the antiplatelet agent dipyridamole has been assessed after inhibiton of thromboxane B₂ (TxB₂) synthesis in 8 patients with confirmed membranous glomerulonephritis. There were three study periods, each of 30 days, and 45 days apart, namely a washout period, treatment with dipyridamole 300 mg/d, and dipyridamole 225 mg/d plus aspirin 150 mg/d. On Days 1 and 30 of each study period serum and urine creatinine, 24-h excretion of protein, creatinine clearance, platelet aggregometry on whole blood and serum TxB₂ were measured. Treatment with dipyridamole alone or with aspirin produced significant inhibition of platelet aggregation and a fall in 24-h protein excretion; the latter amounted to 54% with dipyridamole alone and 56 % with dipyridamole plus aspirin (NS). Dipyridamole plus aspirin caused an 82 % reduction in serum TxB₂.     

Cerivastatin inhibits fetal calf serunvinduced DNA synthesis in cultured rat mesangial cells

SUMMARY: Inhibition of mevalonate synthesis by several statins has been shown to suppress DNA synthesis in glomerular mesangial cells. In the present study, we investigated the effect of a new statin, cerivastatin, on fetal calf serum (FCS)-induced DNA synthesis of cultured rat mesangial cells. Cultured rat mesangial cells were stimulated by 10% FCS in the presence or absence of cerivastatin and mevalonate. 5-bromo-2-deoxyuridine (BrdU) incorporation was used to assess DNA synthesis. the present study showed that 10% FCS caused marked stimulation of DNA synthesis in the mesangial cells. Cerivastatin inhibited FCS-stimulated BrdU incorporation in a dose-dependent manner. IC₅₀ was approximately 1 umol/L. Exogenous mevalonate, farnesyl pyrophosphate and geranylgeranyl pyrophosphate significantly prevented the inhibitory effect of cerivastatin on DNA replication. It appears that cerivastatin, by inhibiting the synthesis of mevalonate, may suppress DNA synthesis in the mesangial cells.